Curcumin and n-acetylcysteine cocrystal produced with supercritical solvent: characterization, solubility, and preclinical evaluation of antinociceptive and anti-inflammatory activities

Paulazzi, A. R.; Alves, Bianca Oliveira; Zilli, Gabriela Adriany Lisboa; Santos, Aline Elias dos; Petry, Fernanda; Soares, Krissie Daian; Danielli, Letícia Jacobi; Pedroso, Jefferson; Apel, Miriam Anders; Aguiar, Gean Pablo S.; Siebel, Anna Maria; Oliveira, J. Vladimir; Müller, Liz Girardi

doi:10.1007/s10787-021-00917-5

Cited by 10 publications

(4 citation statements)

References 72 publications

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“…It is known that polyols can increase the solubility of many poorly soluble compounds [49]. The lower values measured in HCl solutions are consistent with previous observations made by Paulazzi et al for curcumin [50] and Lucas-Abellan et al for hesperetin [51].…”

Section: Resultssupporting

confidence: 91%

Sweeteners Show a Plasticizing Effect on PVP K30—A Solution for the Hot-Melt Extrusion of Fixed-Dose Amorphous Curcumin-Hesperetin Solid Dispersions

Wdowiak,

Tajber,

Miklaszewski

et al. 2024

Pharmaceutics

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The co-administration of curcumin and hesperetin might be beneficial in terms of neuroprotective activity; therefore, in this study, we attempted to develop a fixed-dose formulation comprising these two compounds in an amorphous state. The aim of obtaining an amorphous state was to overcome the limitations of the low solubility of the active compounds. First, we assessed the possibility of using popular sweeteners (erythritol, xylitol, and sorbitol) as plasticizers to reduce the glass transition temperature of PVP K30 to prepare the polymer–excipient blends, which allowed the preparation of amorphous solid dispersions via hot-melt extrusion at a temperature below the original glass transition of PVP K30. Erythritol proved to be the superior plasticizer. Then, we focused on the development of fixed-dose amorphous solid dispersions of curcumin and hesperetin. Powder X-ray diffraction and thermal analysis confirmed the amorphous character of dispersions, whereas infrared spectroscopy helped to assess the presence of intermolecular interactions. The amorphous state of the produced dispersions was maintained for 6 months, as shown in a stability study. Pharmaceutical parameters such as dissolution rate, solubility, and in vitro permeability through artificial membranes were evaluated. The best improvement in these features was noted for the dispersion, which contained 15% of the total content of the active compounds with erythritol used as the plasticizer.

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Section: Resultssupporting

confidence: 91%

Sweeteners Show a Plasticizing Effect on PVP K30—A Solution for the Hot-Melt Extrusion of Fixed-Dose Amorphous Curcumin-Hesperetin Solid Dispersions

Wdowiak,

Tajber,

Miklaszewski

et al. 2024

Pharmaceutics

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“…The technique also allows the use of thermally sensitive materials while also being an ecologically friendly method that does not require the use of harmful solvents. Supercritical fluid technology has been employed for drugs such as curcumin, 121 pyrazinamide, 122 carbamazepine, 123 paracetamol, 124 ketoconazole, 125 theophylline, 54 and indomethacin, 120 and leads to an increase in the dissolution rate of drugs.…”

Section: Solubility and Dissolution Enhancement By Co-crystallizationmentioning

confidence: 99%

Co-crystallization: a green approach for the solubility enhancement of poorly soluble drugs

Bhatia,

Devi

2024

CrystEngComm

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“…For example, triptolide has obvious toxicity and side effects, and the incidence of adverse drug reactions of triptolide is considered to be higher than that of other drugs, including the adverse reactions of the digestive system, nephrotoxicity, and cardiovascular system (Wang, Tian, et al, 2019). In addition, the low solubility of many natural products such as triptolide, epigallocatechin-gallate, and curcumin leads to low bioavailability (Paulazzi et al, 2022;Zhu et al, 2019Zhu et al, , 2022. The stability of oridonin is poor and the half-life is short in vivo (Chen, Luo, et al, 2019).…”

Section: Development Of Natural Productsmentioning

confidence: 99%

The efficacy of natural products for the treatment of nasopharyngeal carcinoma

Ao,

Luo,

Zhang

et al. 2023

Chem Biol Drug Des

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Nasopharyngeal carcinoma (NPC) is a malignant tumor originating in the nasopharyngeal epithelium with a high incidence in southern China and parts of Southeast Asia. The current treatment methods are mainly radiotherapy and chemotherapy. However, they often have side effects and are not suitable for long‐term exposure. Natural products have received more and more attention in cancer prevention and treatment because of their its high efficiency, low toxic side effects, and low toxicity. Natural products can serve as a viable alternative, and this study aimed to review the efficacy and mechanisms of natural products in the treatment of NPC by examining previous literature. Most natural products act by inhibiting cell proliferation, metastasis, inducing cell cycle arrest, and apoptosis. Although further research is needed to verify their effectiveness and safety, natural products can significantly improve the treatment of NPC.

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Curcumin and n-acetylcysteine cocrystal produced with supercritical solvent: characterization, solubility, and preclinical evaluation of antinociceptive and anti-inflammatory activities

Cited by 10 publications

References 72 publications

Sweeteners Show a Plasticizing Effect on PVP K30—A Solution for the Hot-Melt Extrusion of Fixed-Dose Amorphous Curcumin-Hesperetin Solid Dispersions

Sweeteners Show a Plasticizing Effect on PVP K30—A Solution for the Hot-Melt Extrusion of Fixed-Dose Amorphous Curcumin-Hesperetin Solid Dispersions

Co-crystallization: a green approach for the solubility enhancement of poorly soluble drugs

The efficacy of natural products for the treatment of nasopharyngeal carcinoma

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